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Drug Metabolism and Metabolite Identification: Strategies, Techniques, and Case Studies

Speakers: S. Cyrus Khojasteh, PhD (Genentech), Bill Fitch, PhD (PosNeg Consulting), Shichang Miao, PhD (ChemoCentryx), Ryan Takahashi, PhD (Genentech), Raju Subramanian, PhD (Gilead), Shuguang Ma, PhD (Genentech)
Organizers: Shuguang Ma, Shichang Miao
Date: 2/22/2018
Time: 8:30-17:00
Registration fee (USD): Regular: $195; Academic: $125; For unemployed or students: $30; For vendor-show rep: $35; For major-sponsor rep (incl lunch): $0;
Location: SF Bay Area: Foster City Crowne Plaza
Major Sponsor: (2)Molecular Discovery; WuXi AppTec
Vendor show vendors registered to date: (20)Absorption Systems; Alturas Analytics; BioDuro; Bruker; CMIC, Inc.; Covance; Cytovier LLC; Hypha Discovery; Intertek; MicroConstants; Pharmaron; PHARMout Laboratories; PPD; QPS; Quotient Clinical Ltd; SCIEX; Sekisui XenoTech, LLC; Seventh Wave; Waters Corporation; Zef Scientific
Registration deadline:2/22/2018  (it will close sooner if the seating cap is reached)

About the Topic

Metabolism plays a key role in the elimination of drugs and their pharmacokinetics. Identification of the metabolites is a major component in drug metabolism studies and is critical for both drug discovery and drug development.  It requires careful strategic planning, utilization of modern analytical techniques in LCMS and NMR, and in-depth data analysis and interpretation. Deep understanding of the fundamentals of drug metabolism and organic chemistry is essential for a successful metabolite ID scientist.  This workshop will discuss drug metabolizing enzymes, state-of-the-art techniques for generating, detecting, and identifying metabolites, data mining tools and MS/MS spectral interpretation, stage-based approaches for metabolite identification in drug discovery and development, and strategies for metabolites-in-safety testing.

This workshop will cover the following topics:

  • Overview of drug metabolism and drug metabolizing enzymes
  • Metabolite identification overview and metabolite detection techniques
  • Metabolite structure identification by MS/MS and NMR
  • General strategies for metabolite identification in drug discovery and development
  • Metabolite generation techniques
  • First-in-human metabolite profiling and metabolites-in-safety testing strategies

About the Speakers

Dr. S Cyrus Khojasteh leads the Biotransformation Group at Genentech (South San Francisco), and was at Pfizer (Groton, CT) prior to 2000. His research focuses on the mechanisms of biotransformation in drug discovery and development with a particular interest in metabolism mediated by cytochrome P450 and non-cytochrome P450 enzymes. Cyrus received his B.S. from the University of California at Berkeley and his Ph.D. in Medicinal Chemistry from the University of Washington under the direction of Dr. Sidney D. Nelson.

Dr. William Fitch consults in drug metabolism, bioanalysis and mass spectrometry at Stanford University and for local pharmaceutical firms. He received his BS at University of Michigan and his PhD at Stanford. He did postdoctoral stints in biosynthetic chemistry at Yale, synthetic chemistry at Syntex and clinical mass spectrometry at Stanford. His 31 year industrial career focused on applications of mass spectrometry in environmental analysis, agricultural chemical discovery, combinatorial chemistry and pharmaceutical discovery. Dr. Fitch has published 69 papers, articles and book chapters.

Dr. Shichang Miao is currently Vice President, Preclinical Development & Clinical DMPK at ChemoCentryx. Previously, he was a director in the pharmacokinetics and drug metabolism department at Amgen South San Francisco. He worked at Tularik Inc. from 1994 through 2004 (most recently as Associate Director, Analytical Chemistry and Drug Metabolism) until Tularik's acquisition by Amgen. He is the founder and president of Pharmaceutical & BioScience Society International. He holds a PhD in organic chemistry / natural products chemistry from the University of British Columbia (Vancouver, Canada) and conducted his postdoctoral research in biochemistry and protein mass spectrometry.

Dr. Ryan Takahashi is a Scientist in DMPK at Genentech, Inc. In this role, he is responsible for supporting small molecule development programs by investigating and advising on metabolism-related concerns. This has led to research focused on characterizing mechanisms and enzymology of drug biotransformation pathways. He received his PhD. from the Faculty of Pharmaceutical Sciences at the University of British Columbia, where he studied roles for aldo-keto reductase enzymes in anthracycline and androgen metabolism under the supervision of Drs. Wayne Riggs and Ronald Reid.

Dr. Raju Subramanian is a Director and head of pharmacokinetics in the department of Drug Metabolism and Pharmacokinetics at Gilead Sciences. He was a Scientific Director at Amgen in the department of Pharmacokinetics and Drug Metabolism in Thousand Oaks CA and was a Research Fellow at Merck in West Point, PA. He received his Ph. D. in Physical Chemistry from State University of New York at Stony Brook, and had post doctoral training at Department of Physics, College of William and Mary and at Beckman Institute, University of Illinois Urbana-Champaign.

Dr. Shuguang Ma is currently a Principal Scientist in DMPK at Genentech Inc. Previously he was a Senior Principal Scientist at Schering-Plough (now Merck) and a Senior Scientist at Amgen. He received his Ph.D. in Analytical Chemistry from Purdue University under the direction of Professor R. Graham Cooks. He has authored 55 research articles in the peer-reviewed journals and three book chapters, covering broad area of mass spectrometry and its applications.

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